Information BDTX-189 is a potent and selective inhibitor of allostericEGFRandHER2oncogenic mutations with Kd of 0.2 nM, 0.76 nM, 13 nM and 1.2 nM for EGFR, HER2,BLKandRIPK2, reapectively. BDTX-189 exhibits anticancer activity. Targets EGFR (Cell-free assay); HER2 (Cell-free assay); RIPK2 (Cell-free assay); BLK (Cell-free assay) 0.2 nM(Kd); 0.76 nM(Kd); 1.2 nM(Kd); 13 nM(Kd) In vitro BDTX-189 is a potent, selective, irreversible active site inhibitor of the ERBB allosteric mutant oncogene family. BDTX-189 achieves a superior selectivity profile in cell-based assays. In vivo BDTX-189 is differentiated by potent, sustained inactivation of multiple allosteric ERBB mutants in vivo. BDTX-189 achieves dose-dependent regression of allosteric HER2 and EGFR tumors at well-tolerated doses. Cell Research(from reference) Cell lines:A431 cells, H292 cells Incubation Time:0-24 h
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BDTX-189
CAS number:2414572-47-5 molecular formula:C29H29ClN6O4
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| Chinese alias | - | ||
| English alias | HY-136789 | 2-Propenamide, N-[4-[[3-chloro-4-(2-pyridinylmethoxy)phenyl]amino]-7-[2-(4-morpholinyl)ethoxy]-6-quinazolinyl]- | s9786 | Tuxobertinib [USAN] | GTPL11676 | N-(4-((3-chloro-4-(pyridin-2-ylmethoxy)phenyl)amino)-7-(2-morpholinoethoxy)quinazolin-6 | ||
| CAS number | 2414572-47-5 | molecular formula | C29H29ClN6O4 |
| molecular weight | 561.03 g/mol | Exact mass | - |
| PSA | 111.000 Ų | logp | 4.401 |
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